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Assay Detail

CHEMBL639639

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of 1 nM [3H]- N6 -(phenylisopropyl) adenosine binding to Adenosine A1 receptor in rat fat cell membrane
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A1 (CHEMBL318)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.
Shamim MT, Ukena D, Padgett WL, Daly JW.
J Med Chem (1989) 32 : 1231 -1237
PubMed 2724296 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 6.21 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 9.22
CHEMBL160369 1 8.89
CHEMBL158507 1 8.23
CHEMBL274855 1 7.44
CHEMBL321505 1 7.39
CHEMBL62350 8-PHENYL THEOPHYLLINE 1 6.46
CHEMBL418333 1 6.37
CHEMBL8488 1 5.82
CHEMBL157655 1 5.80
CHEMBL281811 1 5.70
CHEMBL22042 1 5.38
CHEMBL20483 1 5.31
CHEMBL1355736 THEOPHYLLINE 4.0 1 5.06
CHEMBL278332 1 4.92
CHEMBL418375 1 4.83
CHEMBL281633 1 4.48
CHEMBL113 CAFFEINE 4.0 1 4.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 0.6 nM 9.22
CHEMBL160369 Ki = 1.3 nM 8.89
CHEMBL158507 Ki = 5.9 nM 8.23
CHEMBL274855 Ki = 36.0 nM 7.44
CHEMBL321505 Ki = 41.0 nM 7.39
CHEMBL62350 8-PHENYL THEOPHYLLINE Ki = 350.0 nM 6.46
CHEMBL418333 Ki = 430.0 nM 6.37
CHEMBL8488 Ki = 1500.0 nM 5.82
CHEMBL157655 Ki = 1600.0 nM 5.80
CHEMBL281811 Ki = 2000.0 nM 5.70
CHEMBL22042 Ki = 4200.0 nM 5.38
CHEMBL20483 Ki = 4900.0 nM 5.31
CHEMBL1355736 THEOPHYLLINE Ki = 8700.0 nM 5.06
CHEMBL278332 Ki = 12000.0 nM 4.92
CHEMBL418375 Ki = 14900.0 nM 4.83
CHEMBL281633 Ki = 33000.0 nM 4.48
CHEMBL113 CAFFEINE Ki = 59000.0 nM 4.23